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All Pharm 1 liners
LECOM 2012 All Pharm 1 liners
| Question | Answer |
|---|---|
| Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs) | Half-life (T1/2) |
| Relates the amount of drug in the body to the plasma concentration | Volume of distribution (VD) |
| Plasma concentration of a drug at a given time | Cp |
| The ratio of the rate of elimination of a drug to its plasma concentration | Clearance (CL) |
| The elimination of drug that occurs before it reaches the systemic circulation | First pass effect |
| The fraction of administered dose of a drug that reaches systemic circulation | Bioavailability (F) |
| When the rate of drug input equals the rate of drug elimination | Steady state |
| Metabolism This step of metabolism makes drug more hydrophilic and hence augments elimination | Phase I |
| Different steps of Phase I | Oxidation, reduction, hydrolysis |
| Inducers of Cytochrome P450 (CYP450) | Barbiturates, phenytoin, carbamazepine, and rifampin |
| Inhibitors of CYP450 | Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit |
| Products of Phase II conjugation | Glucuronate, acetic acid, and glutathione sulfate |
| Constant percentage of substrate metabolized per unit time | First order kinetics |
| Drug elimination with a constant amount metabolized regardless of drug concentration | Zero order kinetics |
| Target plasma concentration times (volume of distribution divided by bioavailability) | Loading dose (Cp*(Vd/F)) |
| Concentration in the plasma times (clearance divided by bioavailability) | Maintenance dose (Cp*(CL/F)) |
| Strength of interaction between drug and its receptor | Affinity |
| Selectivity of a drug for its receptor | Specificity |
| Amount of drug necessary to elicit a biologic effect | Potency |
| Ability of drug to produce a biologic effect | Efficacy |
| Ability of a drug to produce 100% of the maximum response regardless of the potency | Full agonist |
| Ability to produce less than 100% of the response | Partial agonist |
| Ability to bind reversibly to the same site as the drug and without activating the effector system | Competitive antagonist |
| Ability to bind to either the same or different site as the drug | Noncompetitive antagonist |
| Mechanism of action (MOA) utilizes intracellular receptors | Thyroid and steroid hormones |
| MOA utilizes transmembrane receptors | Insulin |
| MOA utilizes ligand gated ion channels | Benzodiazepines and calcium channel blockers |
| Median effective dose required for an effect in 50% of the population | ED50 |
| Median toxic dose required for a toxic effect in 50% of the population | TD50 |
| Dose which is lethal to 50% of the population | LD50 |
| Window between therapeutic effect and toxic effect | Therapeutic index |
| Drug with a high margin of safety | High therapeutic index |
| Drug with a narrow margin of safety | Low therapeutic index |
| Antidotes and agents used in drug overdose Antidote used for lead poisoning | Dimercaprol, EDTA |
| Antidote used for cyanide poisoning | Nitrites |
| Antidote used for anticholinergic poisoning | Physostigmine |
| Antidote used for organophosphate/anticholinesterase poisoning | Atropine, pralidoxime (2-PAM) |
| Antidote used for iron salt toxicity | Deferoxamine |
| Antidote used for acetaminophen (APAP) toxicity | N-acetylcysteine (Mucomyst) |
| Antidote for arsenic, mercury, lead, and gold poisoning | Dimercaprol |
| Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic | Penicillamine |
| Antidote used for heparin toxicity | Protamine |
| Antidote used for warfarin toxicity | Vitamin and Fresh frozen plasma (FFP) |
| Antidote for tissue plasminogen activator (t-PA), streptokinase | Aminocaproic acid |
| Antidote used for methanol and ethylene glycol | Ethanol |
| Antidote used for opioid toxicity | Naloxone (IV), naltrexone (PO) |
| Antidote used for benzodiazepine toxicity | Flumazenil |
| Antidote used for tricyclic antidepressants (TCA) | Sodium bicarbonate |
| Antidote used for carbon monoxide poisoning | 100% O2 and hyperbaric O2 |
| Antidote used for digitalis toxicity | Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic) |
| Antidote used for beta agonist toxicity (eg. Metaproterenol) | Esmolol |
| Antidote for methotrexate toxicity | Leucovorin |
| Antidote for beta-blockers and hypoglycemia | Glucagon |
| Antidote useful for some drug induced Torsade de pointes | Magnesium sulfate |
| Antidote for hyperkalemia | sodium polystyrene sulfonate (Kayexalate) |
| Antidote for salicylate intoxication | Alkalinize urine, dialysis |
| Cancer Chemotherapy Constant proportion of cell population killed rather than a constant number | Log-kill hypothesis |
| Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously | Pulse therapy |
| Toxic effect of anticancer drug can be lessened by rescue agents | Rescue therapy |
| Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates | Allopurinol |
| Pyrimidine analog that causes "Thiamine-less death" given with leucovorin rescue | 5-flouracil (5-FU) |
| Drug used in cancer therapy causes Cushing-like symptoms | Prednisone |
| Side effect of Mitomycin | SEVERE myelosuppression |
| MOA of cisplatin | Alkylating agent |
| Common toxicities of cisplatin | Nephro and ototoxicity |
| Analog of hypoxanthine, needs HGPRTase for activation | 6-mercaptopurine (6-MP) |
| Interaction with this drug requires dose reduction of 6-MP | Allopurinol |
| May protect against doxorubicin toxic by scavenging free radicals | Dexrazoxane |
| Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis | Bleomycin |
| Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm | Testicular cancer |
| MOPP regimen used in Hodgkin's disease (HD) | Mechlorethamine+ oncovorin (vincristine)+ procarbazine, and prednisone |
| ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP | Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine |
| Regimen used for non-Hodgkin's lymphoma | COP (cyclophosphamide, oncovin(vincristine), and prednisone) |
| Regimen used for breast cancer | CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+ |
| Alkylating agent, vesicant that causes tissue damage with extravasation | Mechlorethamine |
| Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis | Cyclophosphamide |
| Prevention of cyclophosphamide induced hemorrhagic cystitis | Hydration and mercaptoethanesulfonate (MESNA) |
| Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation | Vincristine |
| Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase | Paclitaxel (taxol) |
| Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides | Cisplatin |
| Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression | Carboplatin |
| Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine) | L-asparaginase |
| Used for hairy cell leukemia; it stimulates NK cells | Interferon alpha |
| Anti-androgen used for prostate cancer | Flutamide (Eulexin) |
| Anti-estrogen used for estrogen receptor + breast cancer | Tamoxifen |
| Newer estrogen receptor antagonist used in advanced breast cancer | Toremifene (Fareston) |
| Some cell cycle specific anti-cancer drugs | Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide) |
| Some cell cycle non-specific drugs | Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea |
| Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonist | Odansetron, granisetron |
| Nitrosoureas with high lipophilicity, used for brain tumors | Carmustine (BCNU) and lomustine (CCNU) |
| Produces disulfiram-like reaction with ethanol | Procarbazine |
| Endocrine drugs: hypothalamic and pituitary hormones Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors | Octreotide |
| Somatotropin (GH) analog used in GH deficiency (dwarfism) | Somatrem |
| GHRH analog used as diagnostic agent | Sermorelin |
| GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively | Leuprolide |
| GnRH antagonist with more immediate effects, used for infertility | Ganirelix |
| Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia | Bromocriptine |
| Hormone inhibiting prolactin release | Dopamine |
| ACTH analog used for diagnosis of patients with corticosteroid abnormality | Cosyntropin |
| Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis | Desmopressin (DDAVP) |
| Thyroid and anti-thyroid drugs Most widely used thyroid drugs such as Synthroid and Levoxyl contain | L-thyroxine (T4) |
| T3 compound less widely used | Cytomel |
| Anti-thyroid drugs | Thioamides, iodides, radioactive iodine, and ipodate |
| Thioamide agents used in hyperthyroidism | Methimazole and propylthiouracil (PTU) |
| Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy | PTU |
| PTU (propylthiouracil) MOA | Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin |
| Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism | Iodide salts |
| Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy | Radioactive iodine |
| Radio contrast media that inhibits the conversion of T4 to T3 | Ipodate |
| Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3 | Beta-blockers such as propranolol |
| Adrenocorticosteroid and adrenocortical antagonists 3 zones of adrenal cortex and their products | Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens) |
| Pneumonic for 3 zones of adrenal cortex | GFR |
| Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation) | Glucocorticoids |
| Short acting GC's | Cortisone and hydrocortisone (equivalent to cortisol) |
| Intermediate acting GC's | Prednisone, methylprednisolone, prednisolone, and triamcinolone |
| Long acting GC's | Betamethasone, dexamethasone, and paramethasone |
| Mineralocorticoids | Fludrocortisone and deoxycorticosterone |
| Some side effects of corticosteroids | Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis |
| Period of time of therapy after which GC therapy will need to be tapered | 5-7 days |
| Inhibitors of corticosteroids biosynthesis Used for Cushing's syndrome (increased corticosteroid) and sometimes for adrenal function test | Metyrapone |
| Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis | Aminoglutethimide |
| Antifungal agent used for inhibition of all gonadal and adrenal steroids | Ketoconazole |
| Antiprogestin used as potent antagonist of GC receptor | Mifepristone |
| Diuretic used to antagonize aldosterone receptors | Spironolactone |
| Common SE of spironolactone | Gynecomastia and hyperkalemia |
| Gonadal hormones and inhibitors Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss | Estrogen |
| Antiestrogen drugs used for fertility and breast cancer respectively | Clomiphene and tamoxifen |
| Common SE of tamoxifen and raloxifene | Hot flashes |
| Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and currently being tested for treatment of breast cancer (Stars study) | Raloxifene |
| Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy | Diethylstilbestrol (DES) |
| Estrogen mostly used in oral contraceptives (OC) | Ethinyl estradiol and mestranol |
| Anti-progesterone used as abortifacient | Mifepristone (RU-486) |
| Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep) | Combination oral contraceptives (OC) |
| Oral contraceptive available in a transdermal patch | Ortho-Evra |
| Converted to more active form DHT by 5 alpha-reductase | Testosterone |
| 5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness | Finasteride (Proscar and Propecia respectively) |
| Anabolic steroid that has potential for abuse | Nandrolone and stanozolol |
| Anti-androgen used for hirsutism in females | Cyproterone acetate |
| Drug is used with testosterone for male fertility | Leuprolide |
| Pancreatic hormones, antidiabetics, and hyperglycemics Alpha cells in the pancreas | Produce glucagon |
| Beta cells in the pancreas | Produce insulin |
| Beta cells are found | Islets of Langerhans |
| Delta cells in the pancreas | Produce Somatostatin |
| Product of proinsulin cleavage used to assess insulin abuse | C-peptide |
| Exogenous insulin | Little C-peptide |
| Endogenous insulin | Normal C-peptide |
| Very rapid acting insulin, having fastest onset and shortest duration of action | Lispro (Humalog) |
| Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia | Regular (Humulin R) |
| Long acting insulin | Ultralente (humulin U) |
| Ultra long acting insulin, has over a day duration of action | Glargine (Lantus) |
| Major SE of insulin | Hypoglycemia |
| Important in synthesis of glucose to glycogen in the liver | GLUT 2 |
| Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation | GLUT 4 |
| Examples of alpha-glucosidase inhibitors (AGI) | Acarbose, miglitol |
| MOA of AGI's | Act on intestine, delay absorption of glucose |
| SE of AGI's | Flatulence (do not use beano to tx), diarrhea, abdominal cramps |
| Alpha-glucosidase inhibitor associated with elevation of LFT's | Acarbose |
| Amino acid derivative | Nateglinide |
| MOA of nateglinide | Insulin secretagogue |
| Biguanide | Metformin |
| Drugs available in combination with metformin | Glyburide, glipizide, and rosiglitazone |
| MOA of metformin | Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity |
| Most important potential SE of metformin | Lactic acidosis |
| Meglitinide | Repaglinide |
| MOA of repaglinide | Insulin release from pancreas; faster and shorter acting than sulfonylurea |
| First generation sulfonylurea | Chlorpropamide, tolbutamide, tolazamide, etc. |
| Second generation sulfonylurea | Glyburide, glipizide, glimepiride, etc. |
| MOA of both generations | Insulin release from pancreas by modifying K+ channels |
| Common SE of sulfonylureas, repaglinide, and nateglinide | Hypoglycemia |
| Sulfonylurea NOT recommended for elderly because of very long half life | Chlorpropamide |
| Thiazolidinediones | Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market) |
| Reason troglitazone was withdrawn from market | Hepatic toxicity |
| MOA of thiazolindinediones | Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism |
| SE of Thiazolindinediones | Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism |
| Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation | Glucagon |
| Drugs used in bone homeostasis Available bisphosphonates | Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid |
| MOA of Bisphosphonates | Inhibits osteoclast bone resorption |
| Only bisphosphonates available IV | Etidronate |
| Uses of bisphosphonates | Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy |
| Major SE of bisphosphonates | Chemical esophagitis |
| Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia | Etidronate |
| Used for prevention of postmenopausal osteoporosis in women | Estrogen (HRT-Hormone replacement therapy) |
| Increase bone density, also being tested for breast CA tx. | Raloxifene (SERM-selective estrogen receptor modulator) |
| Used intranasally and decreases bone resorption | Calcitonin (salmon prep) |
| Used especially in postmenopausal women, dosage should be 1500 mg | Calcium |
| Vitamin given with calcium to ensure proper absorption | Vitamin D |
| Drugs with important actions on smooth muscle Disease caused by excess ergot alkaloids | St. Anthony's Fire |
| Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides | Autocoids |
| Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea | Zollinger-Ellison Syndrome |
| Drug that causes contraction of the uterus | Oxytocin |
| Distribution of histamine receptors H1, H2, and H3 | Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively |
| Prototype antagonist of H1 and H2 receptors | Diphenhydramine |
| 1st generation antihistamine that is highly sedating | Diphendydramine |
| 1st generation antihistamine that is least sedating | Chlorpheniramine or cyclizine |
| 2nd generation antihistamines | Fexofenadine, loratadine, and cetirizine |
| Generation of antihistamine that has the most CNS effects | First generation due to being more lipid-soluble |
| Major indication for H1 receptor antagonist | Use in IgE mediated allergic reaction |
| Antihistamine that can be used for anxiety and insomnia and is not addictive | hydroxyzine (Atarax) |
| H1 antagonist used in motion sickness | Dimenhydrinate, meclizine, and other 1st generation |
| Most common side effect of 1st generation antihistamines | Sedation |
| Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme. | Terfenadine and astemizole (have been removed from the market) |
| H2 blocker that causes the most interactions with other drugs | Cimetidine |
| Clinical use for H2 blockers | Acid reflux disease, duodenal ulcer and peptic ulcer disease |
| Receptors for serotonin (5HT-1) are located | Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance |
| " 5HT-1d agonist used for migraine headaches " | Sumatriptan, naratriptan, and rizatriptan |
| Triptan available in parenteral and nasal formulation | Sumatriptan |
| H1 blocker that is also a serotonin antagonist | Cyproheptadine |
| 5HT2 antagonist mediate synaptic excitation in the CNS and smooth muscle contraction | Ketanserin, cyproheptadine, and ergot alkaloids (partial agonist of alpha and serotonin receptors) |
| Agents for reduction of postpartum bleeding | Ergonovine and ergotamine |
| Agents used in treatment of carcinoid tumor | Ketanserin cyproheptadine, and phenoxybenzamine |
| "5HT-3 antagonist used in chemotherapeutic induced emesis " | "Ondansetron, granisetron, dolasetron and alosetron " |
| 5ht-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease | Dolasetron |
| DOC of chemo induced nausea and vomiting | Odansetron |
| Drug used in ergot alkaloids overdose, ischemia and gangrene | Nitroprusside |
| Reason ergot alkaloids are contraindicated in pregnancy | Uterine contractions |
| SE of ergot alkaloids | Hallucinations resembling psychosis |
| Ergot alkaloid used as an illicit drug | LSD |
| Dopamine agonist used in hyperprolactinemia | Bromocriptine |
| Peptide causing increased capillary permeability and edema | Bradykinin and histamine |
| Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema | Bradykinin |
| Drug causing depletion of substance P (vasodilator) | Capsaicin |
| Prostaglandins that cause abortions | Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha |
| " Difference between COX 1 and COX 2 " | "COX 1 is found throughout the body and COX 2 is only in inflammatory tissue" |
| Drug that selectively inhibits COX 2 | Celecoxib, valdecoxib, and rofecoxib |
| Inhibitor of lipoxygenase | Zileuton |
| Major SE of zileuton | Liver toxicity |
| Inhibitor of leukotrienes (LTD4) receptors and used in asthma | Zafirlukast and montelukast |
| Used in pediatrics to maintain patency of ductus arteriosis | PGE1 |
| Approved for use in severe pulmonary HTN | PGI2 (epoprostenol) |
| Prostaglandin used in the treatment impotence | Alprostadil |
| Irreversible, nonselective COX inhibitor | Aspirin |
| Class of drugs that reversibly inhibit COX | NSAIDS |
| Primary endogenous substrate for Nitric Oxidase Synthase | Arginine |
| MOA and effect of nitric oxide | Stimulates cGMP which leads to vascular smooth muscle relaxation |
| Long acting beta 2 agonist used in asthma | Salmeterol |
| Muscarinic antagonist used in asthma | Ipratropium |
| MOA action of cromolyn | Mast cell stabilizer |
| Enzyme which theophylline inhibits | Phosphodiesterase |
| Methylxanthine derivative used as a remedy for intermittent claudication | Pentoxifylline |
| Antidote for severe CV toxicity of theophylline | Beta blockers |
| " MOA of corticosteroids" | inhibit phospholipase A2 |
| SE of long term (>5 days) corticosteroid therapy and remedy | Adrenal suppression and weaning slowly, respectively |
| Antimicrobials MOA of quinolones | Inhibit DNA gyrase |
| MOA of penicillin | Block cell wall synthesis by inhibiting peptidoglycan cross-linkage |
| Drug used for MRSA | Vancomycin |
| Vancomycin MOA | Blocks peptidoglycan synthesis |
| Type of resistance found with vancomycin | Point mutation |
| Meningitis prophylaxis in exposed patients | Rifampin |
| Technique used to diagnose perianal itching, and the drug used to treat it | "Scotch tape technique and mebendazole" |
| Two toxicities of aminoglycosides | nephro and ototoxicity |
| DOC for Legionnaires' disease | Erythromycin |
| MOA of sulfonamides | Inhibit dihydropteroate synthase |
| Penicillins active against penicillinase secreting bacteria | Methicillin, nafcillin, and dicloxacillin |
| Cheap wide spectrum antibiotic DOC of otitis media | Amoxicillin |
| Class of antibiotics that have 10% cross sensitivity with penicillins | Cephalosporins |
| PCN active against pseudomonas | Carbenicillin, piperacillin and ticarcillin |
| Antibiotic causing red-man syndrome, and prevention | "Vancomycin, infusion at a slow rate and antihistamines" |
| Drug causes teeth discoloration | Tetracycline |
| MOA of tetracycline | Decreases protein synthesis by inhibiting 30S ribosome |
| Drug that causes gray baby syndrome and aplastic anemia | Chloramphenicol |
| Drug notorious for causing pseudomembranous colitis | Clindamycin |
| DOC for tx of pseudomembranous colitis | Metronidazole |
| Treatment of resistant pseudomembranous colitis | ORAL vancomycin |
| Anemia caused by trimethoprim | Megaloblastic anemia |
| Reason fluoroquinolones are contraindicated in children and pregnancy | Cartilage damage |
| DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas | Metronidazole |
| Treatment for TB patients (think RIPE) | Rifampin, Isoniazid, Pyrazinamide, and Ethambutol |
| Metronidazole SE if given with alcohol | Disulfiram-like reaction |
| Common side effect of Rifampin | Red urine discoloration |
| MOA of nystatin | Bind ergosterol in fungal cell membrane |
| Neurotoxicity with isoniazid (INH) prevented by | Administration of Vit. B6 (pyridoxine) |
| Toxicity of amphotericin | Nephrotoxicity |
| SE seen only in men with administration of ketoconazole | Gynecomastia |
| Topical DOC in impetigo | Topical mupirocin (Bactroban) |
| DOC for influenza A | Amantadine |
| DOC for RSV | Ribavirin |
| DOC for CMV retinitis | Ganciclovir |
| SE for ganciclovir | Neutro, leuko and thrombocytopenia |
| Anti-viral agents associated with Stephen Johnson syndrome Nevirapine, amprenavir HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism | Protease inhibitors |
| Antivirals that are teratogens | Delavirdine, efavirenz, and ribavirin |
| Antivirals associated with neutropenia | Ganciclovir, zidovudine, saquinavir, and interferon |
| HIV med used to reduce transmission during birth | AZT (zidovudine) |
| Drug used for African sleeping sickness | Suramin |
| Drug used in Chagas disease | Nifurtimox |
| Cephalosporins able to cross the BBB | Cefixime (2nd) and 3rd generation |
| Drug used for N. gonorrhea in females | Ceftriaxone |
| Cephalosporin causes kernicterus in neonates | Ceftriaxone or cefuroxime |
| SE of INH | Peripheral neuritis and hepatitis |
| Aminoglycoside that is least ototoxic | Streptomycin |
| Drug used in exoerythrocytic cycle of malaria | Primaquine |
| Oral antibiotic of choice for moderate inflammatory acne | Minocycline |
| Drug of choice for leprosy | Dapsone |
| DOC for herpes and its MOA | Acyclovir and inhibits thymidine kinase Acyclovir and inhibits thymidine kinase |
| Anti-microbials that cause hemolysis in G6PD-deficient patients | Sulfonamides |
| MOA of erythromycin | Inhibition of protein synthesis at the 50s subunit of ribosome |
| Anti-biotic frequently used for chronic UTI prophylaxis | sulfamethoxazole/ trimethoprim |
| Lactam that can be used in PCN allergic patients | Aztreonam |
| SE of imipenem | Seizures |
| Anti-viral with a dose limiting toxicity of pancreatitis | Didanosine |
| Sedative Hypnotics Common side effect of hypnotic agents | Sedation |
| Occurs when sedative hypnotics are used chronically or at high doses | Tolerance |
| The most common type of drug interaction of sedative hypnotics with other depressant medications | Additive CNS depression |
| Benzodiazepines Major effect of benzodiazepines on sleep at high doses | REM is decreased |
| Neurologic SE of benzodiazepines | Anterograde amnesia |
| Reason benzos are used cautiously in pregnancy | Ability to cross the placenta |
| Main route of metabolism for benzodiazepines | Hepatic |
| Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired) | Lorazepam, oxazepam, and temazepam |
| "MOA for benzodiazepines " | increase the FREQUENCY of GABA-mediated chloride ion channel opening |
| Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects) | Flumazenil |
| Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin | Diazepam |
| Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia | Clonazepam |
| Benzodiazepines that are the most effective in the treatment of panic disorder | Alprazolam and Clonazepam |
| "Benzodiazepine that is used for anesthesia " | Midazolam |
| DOC for status epilepticus | Diazepam |
| Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs | Chlordiazepoxide and Diazepam |
| Agents having active metabolites, long half lives, and a high incidence of adverse effects | Diazepam, Flurazepam, chlordiazepoxide, and clorazepate |
| Barbiturates Barbiturates may precipitate this hematologic condition | Acute intermittent porphyria |
| Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property | Liver enzyme INDUCTION |
| Barbiturates MOA | Increase the DURATION of GABA-mediated chloride ion channels |
| Barbiturate used for the induction of anesthesia | Thiopental |
| Alcohols Important drug interaction with chloral hydrate | May displace coumadin from plasma proteins |
| Others Site of action for zaleplon and zolpidem | Benzodiazepine receptor BZ1 (although are not considered benzodiazepines) |
| Good hypnotic activity with less CNS SE than most benzodiazepines | Zolpidem, zaleplon |
| Agent that is a partial agonist for the 5-HT1A receptor | Buspirone |
| Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety | Buspirone |
| Alcohols Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS) | Ethanol |
| Agent with zero-order kinetics | Ethanol |
| Rate limiting step of alcohol metabolism | Aldehyde dehydrogenase |
| System that increases in activity with chronic exposure and may contribute to tolerance | MEOS |
| Agent that metabolize acetaldehyde to acetate | Aldehyde dehydrogenase |
| Agents that inhibit alcohol dehydrogenase | Disulfiram, metronidazole, certain sulfonylureas and cephalosporins |
| Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension | Disulfiram |
| The most common neurologic abnormality in chronic alcoholics | Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI) |
| Agent that is teratogen and causes a fetal syndrome | Alcohol |
| Agent that is the antidote for methanol overdose | Alcohol |
| Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure | Fomepizole |
| Anti seizure Drugs Most frequent route of metabolism | Hepatic enzymes |
| Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine | Sodium blockade |
| MOA for benzodiazepines and barbiturates | GABA-related targets |
| MOA for Ethosuximide | Calcium channels |
| MOA for Valproic acid at high doses | Affect calcium, potassium, and sodium channels |
| Drugs of choice for generalized tonic-clonic and partial seizures | Valproic acid and Phenytoin |
| DOC for febrile seizures | Phenobarbital |
| Drugs of choice for absence seizures | Ethosuximide and valproic acid |
| Drug of choice for myoclonic seizures | Valproic acid |
| Drugs of choice for status epilepticus | IV diazepam or phenytoin (for prolonged therapy not acute) |
| Drugs that can be used for infantile spasms | Corticosteroids |
| Anti-seizure drugs used also for bipolar affective disorder (BAD) | Valproic acid, carbamazepine, phenytoin and gabapentin |
| Anti-seizure drugs used also for Trigeminal neuralgia | Carbamazepine |
| Anti-seizure drugs used also for pain of neuropathic orgin | Gabapentin |
| Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism | Phenytoin |
| SE of phenytoin | Gingival hyperplasia, nystagmus, diplopia and ataxia |
| Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida | Carbamazepine |
| Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress | Valproic acid |
| Laboratory value required to be monitored for patients on valproic acid | Serum ammonia and LFT's |
| SE for Lamotrigine | Stevens-Johnson syndrome |
| SE for Felbamate | Aplastic anemia and acute hepatic failure |
| Anti-seizure medication also used in the prevention of migraines | Valproic acid |
| Carbamazepine may cause | Agranulocytosis |
| Anti-seizure drugs used as alternative drugs for mood stabilization | Carbamazepine, gabapentin, lamotrigine, and valproic acid |
| General Anesthetics MOA of general anesthetics | Unclear, thought to increase the threshold for firing of CNS neurons |
| Inhaled anesthetic with a low blood/gas partition coefficient | Nitrous oxide |
| Inversely related to potency of anesthetics | Minimum alveolar anesthetic concentration (MAC) |
| Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents | Halothane and methoxyflurane |
| Most inhaled anesthetics SE | Decrease arterial blood pressure |
| Inhaled anesthetics are myocardial depressants | Enflurane and halothane |
| Inhaled anesthetic causes peripheral vasodilation | Isoflurane |
| Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis | Halothane |
| Inhaled anesthetics, less likely to lower blood pressure than other agents, and has the smallest effect on respiration | Nitrous oxide |
| Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency | Methoxyflurane |
| Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia | Nitrous oxide |
| Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm | Desflurane |
| DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics | Dantrolene |
| IV barbiturate used as a pre-op anesthetic | Thiopental |
| Benzodiazepine used adjunctively in anesthesia | Midazolam |
| Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose | Flumazenil |
| This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery | Ketamine |
| Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia | Fentanyl |
| State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide | Neuroleptanesthesia |
| Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension | Propofol |
| Local Anesthetics MOA of local anesthetics (LA's) | Block voltage-dependent sodium channels |
| This may enhance activity of local anesthetics | Hyperkalemia |
| This may antagonize activity of local anesthetics | Hypercalcemia |
| Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity | Vasodilation |
| Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery | Cocaine |
| Longer acting local anesthetics which are less dependent on vasoconstrictors | Tetracaine and bupivacaine |
| These LA's have surface activity | Cocaine and benzocaine |
| Most important toxic effects of most local anesthetics | CNS toxicity |
| Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction | Cocaine |
| LA causing methemoglobinemia | Prilocaine |
| Skeletal Muscle Relaxants Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation | Neuromuscular blocking drugs |
| These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB) | Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic |
| These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine) | Nondepolarizing type antagonists |
| Agent with long duration of action and is sost likely to cause histamine release | Tubocurarine |
| Non-depolarizing antagonist has short duration | Mivacurium |
| Agent can blocking muscarinic receptors | Pancuronium |
| Agent undergoing Hofmann elimination (breaking down spontaneously) | Atracurium |
| One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, xcuses muscle pain postoperatively and myoglobinuria may occur | Succinylcholine |
| During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine | Cholinesterase inhibitors |
| Spasmolytic drugs Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease | Spasmolytic drugs |
| Facilitates GABA presynaptic inhibition | Diazepam |
| GABA agonist in the spinal cord | Baclofen |
| Similar to clonidine and may cause hypotension | Tizanidine |
| DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle | Dantrolene |
| Agent used for acute muscle spasm | Cyclobenzaprine |
| Drugs Used in Parkinsonism & Other Movement Disorders Antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible | Drug induced Parkinsonism |
| Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB | L-dopa |
| This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias) | Carbidopa |
| Clinical response that may fluctuate in tx of Parkinson's dx | "On-off-phenomenon" |
| Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma | Levodopa |
| Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia | Bromocriptine |
| Non ergot agents used as first-line therapy in the initial management of Parkinson's | Pramipexole and ropinirole |
| Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis | Amantadine |
| Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt's | Selegiline |
| Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's) | Entacapone and Tolcapone |
| Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects | Benztropine |
| Agent effective in physiologic and essential tremor | Propranolol |
| Agents used in Huntington's Disease | Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic) |
| Agents used in Tourette's dx | Haloperidol or pimozide |
| Chelating agent used in Wilson's disease | Penicillamine |
| Antipsychotics Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor | Older antipsychotic agents, D2 receptors |
| Side effects occuring in antipsychotics that block dopamine | Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain |
| Antipsychotics that reduce positive symptoms only | Older antipsychotics |
| Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation | Olanzapine, aripiprazole, and sertindole |
| Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia | Risperidone |
| Atypical antipsychotic causing high prolactin levels | Risperidone |
| Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes | Olanzapine |
| Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker | Haloperidol |
| Drug used in neuroleptic malignant syndrome | Dantrolene |
| Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment) Muscarinic blockers Antipsychotic having the strongest autonomic effects | Thioridazine |
| Antipsychotic having the weakest autonomic effects | Haloperidol |
| Antipsychotic that does not block muscarinic or histamine receptors, and it prolongs the QT interval | Sertindole |
| Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias | Thioridazine |
| Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause agranulocytosis | Clozapine |
| Anti-psychotic not shown to cause tardive dyskinesia | Clozapine |
| Anti-psychotics available in depot preparation | Fluphenazine and haloperidol |
| Reduced seizure threshold | Low-potency typical antipsychotics and clozapine |
| Orthostatic hypotension and QT prolongation | Low potency and risperidone |
| Increased risk of developing cataracts | Quetiapine |
| Lithium Major route of elimination for Lithium | Kidneys |
| Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop | Lithium toxicity |
| Drug increases the renal clearance hence decreases levels of lithium | Theophylline |
| Lithium is associated with this congenital defect | Cardiac anomalies and is contraindicated in pregnancy or lactation |
| DOC for bipolar affective disorder | Lithium |
| SE of lithium | Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus |
| Antidepressants Example of three antidepressants that are indicated for obsessive compulsive disorder | Clomipramine, fluoxetine and fluvoxamine |
| Neurotransmitters affected by the action of antidepressants | Norepinephrine and serotonin |
| Usual time needed for full effect of antidepressant therapy | 2 to 3 weeks |
| Population group especially sensitive to side effects of antidepressants | Elderly patients |
| All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion | Side-effect profile and prior pt response |
| Well-tolerated and are first-line antidepressants | SSRI's, bupropion, and venlafaxine |
| Monoamine oxidase inhibitors (MAOI) Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression | Monamine oxidase inhibitors |
| Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats) | Hypertensive crisis |
| MAOI should not be administered with SSRI's or potent TCA's due to development of this condition | Serotonin syndrome |
| Tricyclic antidepressants (TCA) Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly | Tricyclic antidepressants (TCA) |
| Three C's associated with TCA toxicity | Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS) |
| Agents having higher sedation and antimuscarinic effects than other TCA's | Tertiary amines |
| TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects | Amitriptyline |
| TCA used in chronic pain, enuresis, and ADD | Imipramine |
| TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep | Doxepin |
| TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms | Clomipramine |
| Secondary amines that have less sedation and more excitation effect | Nortriptyline, Desipramine |
| Heterocyclics Antidepressant associated with neuroleptic malignant syndrome | Amoxapine |
| Antidepressant associated with seizures and cardiotoxicity | Maprotiline |
| Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure | Venlafaxine |
| Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake | Venlafaxine |
| Antidepressant also used for sleep that causes priapism | Trazodone |
| Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure | Nefazodone |
| Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures | Bupropion |
| Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating | Mirtazapine |
| SE of mirtazapine | Liver toxicity, increased serum cholesterol |
| Selective serotonin reuptake inhibitors (SSRI) Except for these agents all SSRI have significant inhibition of CytP450 enzymes | Citalopram and its metabolite escitalopram |
| SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx | Fluoxetine |
| SSRI indicated for premenstrual dysphoric disorder | Fluoxetine (Sarafem) |
| Some of SSRIs' therapeutic effects beside depression | Panic attacks, social phobias, bulimia nervosa, and PMDD premenstrual dysphoric disorder), OCD |
| SSRI's less likely to cause a withdrawal syndrome | Fluoxetine |
| Opioid Analgesics & Antagonists Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons | Ascending pathways |
| Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release | Presynaptic mu, delta, and kappa receptors |
| Activation of these receptors open K+ ion channels to cause membrane hyperpolarization | Postsynaptic Mu receptors |
| Tolerance to all effects of opioid agonists can develop except | Miosis and constipation |
| All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction | Meperidine |
| SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone | Opioid Analgesics |
| Strong opioid agonists | Morphine, methadone, meperidine, and fentanyl |
| Opioids used in anesthesia | Morphine and fentanyl |
| Opioid used in the management of withdrawal states | Methadone |
| Opioid available trans-dermally | Fentanyl |
| Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema | Morphine |
| Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome | Meperidine |
| Moderate opioid agonists | Codeine, hydrocodone, and oxycodone |
| Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures | Propoxyphene |
| Partial agonist or mixed antagonists Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal | Buprenorphine |
| Opioid antagonist that is given IV and had short DOA | Naloxone |
| Opioid antagonist that is given orally in alcohol dependency programs | Naltrexone |
| These agents are used as antitussive | Dextromethorphan, Codeine |
| These agents are used as antidiarrheal | Diphenoxylate, Loperamide |
| Drugs of Abuse Inhalant anesthetics | NO, chloroform, and diethyl ether |
| Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation | Fluorocarbons and Industrial solvents |
| Cause dizziness, tachycardia, hypotension, and flushing | Organic nitrites |
| Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression | Steroids |
| Readily detected markers that may assist in diagnosis of the cause of a drug overdose include | Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses |
| Opioid Analgesics Most commonly abused in health care professionals | Heroin, morphine, oxycodone, meperidine and fentanyl |
| This route is associated with rapid tolerance and psychologic dependence | IV administration |
| Leads to respiratory depression progressing to coma and death | Overdose of opioids |
| Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome | Abstinence syndrome |
| Treatment for opioid addiction | Methadone, followed by slow dose reduction |
| This agent may cause more severe, rapid and intense symptoms to a recovering addict | Naloxone |
| Sedative-Hypnotics Sedative-Hypnotics action | Reduce inhibition, suppress anxiety, and produce relaxation |
| Additive effects when Sedative-Hypnotics used in combination with these agents | CNS depressants |
| Common mechanism by which overdose result in death | Depression of medullary and cardiovascular centers |
| "Date rape drug" | Flunitrazepam (rohypnol) |
| The most important sign of withdrawal syndrome | Excessive CNS stimulation (seizures) |
| Treatment of withdrawal syndrome involves | Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol |
| These agents are CNS depressants | Ethanol, Barbiturates, and Benzodiazepines |
| Stimulants Withdrawal from this drug causes lethargy, irritability, and headache | Caffeine |
| W/D from this drug causes anxiety and mental discomfort | Nicotine |
| Treatments available for nicotine addiction | Patches, gum, nasal spray, psychotherapy, and bupropion |
| Chronic high dose abuse of nicotine leads to | Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures |
| Tolerance is marked and abstinence syndrome occurs | Amphetamines |
| Amphetamine agents | Dextroamphetamines and methamphetamine |
| These agents are congeners of Amphetamine | DOM, STP, MDA, and MDMA "ecstasy" |
| Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke) | Cocaine "super-speed" |
| Hallucinogens Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of both horizontal and vertical nystagmus is pathognomonic | PCP |
| Removal of PCP may be aided | Urinary acidification and activated charcoal or continual nasogastric suction |
| THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur | Marijuana |
| This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention | Bethanechol |
| Only direct acting agent that is very lipid soluble and used in glaucoma | Pilocarpine |
| This agent used to treat dry mouth in Sjögren's syndrome | Cevimeline |
| Indirect-Acting ACh Agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis | Edrophonium |
| Carbamate with intermediate action postoperative and neurogenic ileus and urinary retention | Neostigmine |
| Treatment of atropine overdose and glaucoma (because lipid soluable). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions | Physostigmine |
| Treatment of myasthenia gravis | Pyridostigmine |
| Organophosphates Antiglaucoma organophosphate | Echothiophate |
| Associated with an increased incidence of cataracts in patients treated for glaucoma | Long acting cholinesterase inhibitors |
| Scabicide organophosphate | Malathion |
| Organophosphate anthelmintic agent with long DOA | Metrifonate |
| Toxicity of organophosphate: | DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating) |
| The most important cause of acute deaths in cholinesterase inhibitor toxicity | Respiratory failure |
| The most toxic organophosphate | Parathion |
| Treatment of choice for organophosphate overdose | Atropine |
| This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure | Pralidoxime |
| Cholinoreceptor Blockers & Cholinesterase Regenerators Prototypical drug is atropine | Nonselective Muscarinic Antagonists |
| Treat manifestations of Parkinson's disease and EPS | Benztropine, trihexyphenidyl |
| Treatment of motion sickness | Scopolamine |
| Produce mydriasis and cycloplegia | Atropine, homatropine tropicamide |
| Bronchodilation in asthma and COPD | Ipratropium |
| Reduce transient hyper GI motility | Dicyclomine, methscopolamine |
| Cystitis, postoperative bladder spasms, or incontinence | Oxybutynin, dicyclomine |
| Toxicity of anticholinergics | block SLUD (salivation, lacrimation, urination, defecation |
| Another pneumonic for anticholinergic toxicity | "dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat" |
| Atropine fever is the most dangerous effect and can be lethal in this population group | Infants |
| Contraindications to use of atropine | Infants, closed angle glaucoma, prostatic hypertrophy |
| Nicotinic Antagonists Prototype ganglion blocker | Hexamethonium |
| Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate | Severe hypertension |
| Reversal of blockade by neuromuscular blockers | Cholinesterase inhibitors |
| Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agent, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis | Nondepolarizing Neuromuscular Blockers |
| Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use | Succinylcholine |
| Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred) | Cholinesterase Regenerators |
| Used to treat patients exposed to insecticides such as parathion | Pralidoxime |
| Sympathomimetics Pneumonic for beta receptors | You have 1 heart (Beta 1) and 2 lungs (Beta 2) |
| This is the drug of choice for anaphylactic shock | Epinephrine |
| Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction | Amphetamines |
| Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia | Phenylephrine |
| Epinephrine and dipivefrin are used for | Glaucoma |
| Newer alpha 2 agonist (apraclonidine and brimonidine) treat glaucoma | Reduce aqueous synthesis |
| Short acting Beta 2 agonists that is drug of choice in treatment of acute asthma but not recommended for prophylaxis | Albuterol |
| Longer acting Beta 2 agonists is recommended for prophylaxis of asthma | Salmeterol |
| These agents increase blood flow and may be beneficial in treatment of acute heart failure and some types of shock | Beta1 agonists |
| These agents decrease blood flow or increase blood pressure, are local decongestant, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion | Alpha1 agonists |
| Shock due to septicemia or myocardial infarction is made worse by | Increasing afterload and tissue perfusion declines |
| Often mixed with local anesthetic to | Reduce the loss from area of injection |
| Chronic orthostatic hypotension can be treated with | Midodrine |
| Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus | Terbutaline |
| Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis | Ephedrine |
| Alpha 1 agonist toxicity | Hypertension |
| Beta 1 agonist toxicity | Sinus tachycardia and serious arrhythmias |
| Beta 2 agonist toxicity | Skeletal muscle tremor |
| The selective agents loose their selectivity at | high doses |
| Adrenoceptor Blocker Nonselective alpha-blocking drug, long acting and irreversible, and used to treat pheochromocytoma. Blocks 5-HT, so occasionaly used for carcinoid tumor. Blocks H1 and used in mastocytosis | Phenoxybenzamine |
| Nonselective alpha-blocking drug, short acting and reversible, used for rebound HTN from rapid clonidine withdrawal, and Raynaud's phenomena | Phentolamine |
| Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension | Prazosin, terazosin, doxazosin |
| Selective Alpha 2 blocker used for impotence (controversial effectiveness) | Yohimbine |
| Beta-Blocking Drugs SelectiveB1 Receptor blockers that may be useful in treating patients with asthma | Acebutolol, atenolol, esmolol, metoprolol |
| Combined alpha and beta blocking agents that may have application in treatment of CHF | Labetalol and carvedilol |
| Beta blockers partial agonist activity (intrinsic sympathomimetic activity) cause some bronchodilation and may have an advantage in treating patients with asthma | Pindolol and acebutolol |
| This beta blocker lacks local anesthetic activity (decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma | Timolol |
| This parenteral beta blocker is a short acting | Esmolol |
| This beta blocker is the longest acting | Nadolol |
| These beta blockers are less lipid soluble | Acebutolol and atenolol |
| This beta blocker is highly lipid soluble and may account for side effects such as nightmares | Propranolol |
| Clinical uses of these agents include treatment of HTN, angina, arrhythmias, and chronic CHF | Beta blockers |
| Toxicity of these agents include bradycardia, AV blockade, exacerbation of acute CHF, signs of hypoglycemia may be masked (tachycardia, tremor, and anxiety) | Beta blockers |
| Glaucoma (all agents topical except for diuretics) Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction | Pilocarpine, carbachol, physostigmine |
| Nonselective alpha agonists that increases outflow, probably via the uveoscleral veins | Epinephrine, dipivefrin |
| Selective alpha agonists that decreases aqueous secretion | Apraclonidine, brimonidine |
| These Beta blockers decrease aqueous secretion | Timolol (nonselective), betaxolol (selective) |
| This diuretic decreases aqueous secretion due to lack of HCO3- ion. Causes drowsiness and paresthesias, alkalinization of the urine may precipitate calcium salts, hypokalemia, acidosis | Acetazolamide |
| This agent cause increased aqueous outflow | Prostaglandin PGF2a |
| Antihypertensive Agents Inhibit angiotensin-converting enzyme (ACE) | Ace inhibitors |
| Captopril and enalapril (-OPRIL ending) are | Ace inhibitors |
| SE of ACE inhibitors | Dry cough, hyperkalemia |
| Ace inhibitors are contraindicated in | pregnancy and with K+ |
| Losartan and valsartan block | Angiotensin receptor |
| Angiotensin receptor blockers do NOT cause | Dry cough |
| Block L-type calcium channel | Calcium channel blockers |
| CCB contraindicated in CHF | Verapamil |
| CCB with predominate effect on arteriole dilation | Nifedipine |
| SE of CCB | Constipation, edema, and headache |
| Reduce heart rate, contractility, and O2 demand | Beta-blockers |
| B-blockers that are more cardioselective | Beta C2001-selective blockers |
| Cardioselective Beta 1-blockers | Atenolol, acebutolol, and metoprolol |
| Beta-blockers should be used cautiously in | Asthma (bronchospastic effects), diabetes (block signs of hypoglycemia) and peripheral vascular disease |
| Non-selective Beta-blocker also used for migraine prophylaxis | Propranolol |
| SE of beta blockers | Bradycardia, SEXUAL DYSFUNCTION, decrease in HDL, and increase in Triglycerols (TG) |
| Alpha 1selective blockers | Prazosin, terazosin and doxazosin (-AZOSIN ending) |
| Non-selective Alpha1blockers use to treat pheochromocytoma | Phenoxybenzamine |
| For rebound HTN from rapid clonidine withdrawal | Phentolamine |
| A1a-selective blocker used for BPH | Tamsulosin (Flomax) |
| SE of alpha blockers | Orthostatic hypotension (especially with first dose) and reflex tachycardia |
| Presynaptic Alpha 2 agonist used in HTN | Clonidine, and methyldopa |
| SE of methyldopa | Positive Comb's test, depression |
| Methyldopa is contraindicated in | Geriatrics due to its CNS (depression) effects |
| SE of clonidine | Rebound HTN, sedation, dry mouth |
| Ganglionic blockers formerly used in HTN | Trimethaphan, and hexamethonium |
| Direct vasodilator of arteriolar smooth muscle | Hydralazine |
| SE of hydralazine | Lupus-like syndrome |
| Arterial vasodilator that works by opening K+ channels | Minoxidil |
| SE of minoxidil | Hypertrichosis |
| IV Drug used Hypertensive Crisis | Nitroprusside |
| Nitroprusside vasodilates | Arteries and veins |
| Toxicity caused by nitroprusside and treatment | Cyanide toxicity treated with sodium thiosulfate |
| Diuretics Carbonic anhydrase inhibitor | Acetazolamide |
| Diuretic used for mountain sickness and glaucoma | Acetazolamide |
| SE of acetazolamide | Paresthesias, alkalization of the urine (which may ppt. Ca salts), hypokalemia, acidosis, and encephalopathy in patients with hepatic impairment |
| MOA of loop diuretics | inhibits Na+/K+/2Cl- cotransport |
| Site of action of loop diuretics | Thick ascending limb |
| SE of loop (furosemide) diuretics | Hyperuricemia, hypokalemia and ototoxicity |
| Aminoglycosides used with loop diuretics potentiate adverse effect | Ototoxicity |
| Loops lose and thiazide diuretics retain | Calcium |
| MOA of thiazide diuretics | Inhibit Na+/Cl- cotransport |
| Site of action of thiazide diuretics | Work at early distal convoluted tubule |
| Class of drugs that may cause cross-sensitivity with thiazide diuretics | Sulfonamides |
| SE of thiazide (HCTZ) diuretics | Hyperuricemia, hypokalemia and hyperglycemia |
| Potassium sparing diuretics inhibit | Na+/K+ exchange |
| Diuretic used to treat primary aldosteronism | Spironolactone |
| SE of spironolactone | Gynecomastia hyperkalemia, and impotence |
| Osmotic diuretic used for increased intracranial pressure | Mannitol |
| Antidiuretic hormone (ADH) agonist and antagonist ADH agonist used for pituitary diabetes insipidus | Desmopressin (DDAVP) |
| Used for SIADH | Demeclocycline |
| SE of demeclocycline | Bone marrow and teeth discoloration for children under 8 years of age |
| Antiarrhythmic agents MOA of class I A (eg. Procainamide), class IB (eg. Lidocaine), and class IC (eg. Flecainide) antiarrhythmics | Sodium channel blockers |
| SE of procainamide | Lupus-like syndrome |
| Limiting side effect of Quinidine | Prolongs QT interval |
| Other side effects of Quinidine | Thrombocytopenic purpura, and CINCHONISM |
| Major drug interaction with Quinidine | Increases concentration of Digoxin |
| DOC for management of acute Ventricular arrhythmias | Lidocaine |
| DOC for digoxin induced arrhythmias | Phenytoin |
| SE of phenytoin | Gingival hyperplasia |
| Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as last line agents | Class IC (flecainide, propafenone, moricizine) |
| Class II antiarrhythmics are | B-blockers |
| Antiarrhythmic that exhibits Class II and III properties | Sotalol |
| Side effect of sotalol | prolongs QT and PR interval |
| Used intravenously for acute arrhythmias during surgery | Esmolol |
| Anti-arrhythmics that decrease mortality | B-blockers |
| MOA of class III antiarrhythmics | Potassium channel blockers |
| Class III antiarrhythmic that exhibits properties of all 4 classes | Amiodarone |
| Specific pharmacokinetic characteristic of amiodarone | Prolonged half-life, up to six weeks |
| Antiarrhythmic effective in most types of arrhythmia | Amiodarone |
| SE of Amiodarone | Dysfunction, photosensitivity, skin (blue smurf syndrome), Pulmonary fibrosis, thyroid and corneal deposits |
| MOA of class IV antiarrhythmics | Calcium channel blockers |
| Life threatening cardiac event that prolong QT leads to | Torsades de pointes |
| Agent to treat torsades de pointes | Magnesium sulfate |
| Drug used supraventricular arrhythmias | Digoxin |
| DOC for paroxysmal supraventricular tachycardia (PSVT) | Adenosine |
| Adenosine's MOA | Activates acetylcholine sensitive K+ channels in SA and AV node |
| Anti-arrhythmic with 15 second duration of action | Adenosine |
| Vasodilators and treatment of angina MOA of sildenafil (Viagra) | Inhibits phosphodiesterase-5, enhancing effects of nitric oxide-activated increases in cGMP |
| Drugs used in the management of angina | Aspirin, Nitrates, CCB, and Beta blockers |
| Aspirin reduces mortality in unstable angina by | Platelet aggregation inhibition |
| MOA of nitrates | Relax vascular smooth muscle, at low doses dilate veins and at high doses dilate arterioles |
| Nitrate used for acute anginal attacks | Nitroglycerin sublingual tablets |
| Nitrate used to prevent further attacks | Oral and transdermal forms of nitroglycerin |
| Nitrate free intervals are needed due to | Tolerance |
| SE of nitrates | Postural hypotension, reflex tachycardia, hot flashes, and throbbing headache due to meningeal artery dilation |
| CCB are DOC for | Prinzmetal's angina |
| Beta blockers are used for which type of anginal attack | Classic |
| Drugs used to treat CHF MOA of Cardiac glycosides (eg. digoxin) | Indirectly increase intracellular calcium and cardiac contractility by inhibit Na+/K+ ATPase |
| Digoxin is used in | Atrial fibrillation and CHF |
| Digoxin toxicity can be precipitated by | Hypokalemia |
| Antidote for digoxin toxicity | Digibind |
| Phosphodiesterase inhibitors that increase mortality and have been found to have NO beneficial effects | Amrinone and milrinone |
| SE of amrinone | Thrombocytopenia |
| Beta 1 agonists used in acute CHF | Dobutamine and dopamine |
| Diuretics work in CHF by | Reducing preload |
| Beta blockers work in CHF by | Reducing progression of heart failure (never use in acute heart failure) |
| Agent used in CHF that is a selective alpha and nonselective beta blocker | Carvedilol |
| Agent used in acutely decompensated CHF resembling natriuretic peptide | Nesiritide (Natrecor) |
| Drugs used in coagulation disorders Vitamin K dependent anticoagulant | Warfarin (PT) |
| Warfarin is contraindicated in | Pregnancy |
| Anticoagulant of choice in pregnancy | Heparin |
| Heparin (PTT) increases activity of | Antithrombin 3 |
| Route of administration of warfarin | Oral |
| Routes of administration of heparin | IM (only LMW) and IV |
| SE of both warfarin and heparin | Bleeding |
| SE of heparin | Heparin induced thrombocytopenia (HIT) |
| Alternative anticoagulant used if HIT develops | Lepirudin |
| Antidote to reverse actions of warfarin | Vitamin K or fresh frozen plasma |
| Antidote to reverse actions of heparin | Protamine sulfate |
| MOA of aspirin | Irreversibly blocking cyclooxygenase |
| Agent used to treat MI and to reduce incidence of subsequent MI | Aspirin |
| SE of Aspirin | GI bleeding |
| Antiplatelet drug reserved for patients allergic to aspirin | Ticlopidine |
| SE for ticlopidine | Neutropenia and agranulocytosis |
| Effective in preventing TIA's | Clopidogrel and ticlopidine |
| Prevents thrombosis in patients with artificial heart valve | Dipyridamole |
| Block glycoprotein IIb/IIIa involved in platelet cross-linking | Abciximab, tirofiban and eptifibatide |
| MOA of thrombolytics | Degradation of fibrin clots and are administered |
| Thrombolytics are used for | Pulmonary embolism and DVT |
| Thrombolytic that can cause allergic reaction | Streptokinase |
| Thrombolytic used for acute MI and ischemic (non hemorrhagic) CVA | Tissue plasmin activator |
| SE of tPA | Cerebral hemorrhage |
| Antidote for thrombolytics | Aminocaproic acid |
| Agents used in anemias and hematopoietic growth factors Agent to treat hypochromic microcytic anemias | Ferrous sulfate |
| Chelating agent used in acute iron toxicity | Deferoxamine |
| Agent for pernicious anemia | Cyanocobalamin (Vit B12) |
| Agent used for neurological deficits in megaloblastic anemia | Vitamin B12 |
| Agent used for megaloblastic anemia (but does NOT reverse neurologic symptoms) and decrease neural tube defects during pregnancy | Folic acid |
| Agent used for anemias associated with renal failure | Erythropoietin |
| Agent used neutropenia especially after chemotherapy | G-CSF (filgrastim) and GM-CSF (sargramostim) |
| Treatment of patients with prior episodes of thrombocytopenia after a cycle of cancer chemotherapy | Interleukin 11 (oprelvekin) |
| Antihyperlipidemics Decrease intestinal absorption of cholesterol | Bile acid-binding resins |
| Cholestyramine and colestipol are | Bile acid-binding resins |
| Major nutritional side effect of bile acid-binding resins | Impair absorption of fat soluble vitamin absorption (A,D,E,K) |
| MOA of lovastatin (STATIN) | inhibits HMG COA reductase |
| HMG CoA reductase inhibitors are contraindicated in | Pregnancy |
| Drug or foods (grapefruit juice) that increase statin effect | Inhibit Cytochrome P450 3A4 |
| SE of HMG COA reductase inhibitors | Rhabdomyolysis and Hepatotoxicity |
| Monitoring parameter to obtain before initiation of STATINS | LFT's |
| Decreases liver triglycerol synthesis | Niacin |
| SE of niacin | Cutaneous flush |
| Cutaneous flush and be reduced by pretreatment with | Aspirin |
| Fibrates (gemfibrozil) increase activity of | Lipoprotein lipase |
| Most common SE of fibrates | Nausea |
| Fibrates are contraindicated in | Pregnancy |
| Concurrent use of fibrates and statins increases risk of | Rhabdomyolysis |
| New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with the Statins | Ezetimibe (Zetia) |
| NSAIDS and DMARDS MOA of NSAIDS | inhibit prostaglandin synthesis by inhibiting cyclo-oxygenase (cox) |
| Difference between aspirin and other NSAIDS | Aspirin irreversibly inhibits cyclooxygenase |
| Four main actions of NSAIDS | Anti-inflammatory, analgesia, antipyretic and antiplatelet activity |
| Agent used for closure of patent ductus arteriosus | Indomethacin |
| Aspirin is contraindicated in children with viral infection | Potential for development of Reye's syndrome |
| SE of salicylates | Tinnitus, GI bleeding |
| NSAID also available as an ophthalmic preparation | Diclofenac |
| NSAID available orally, IM and ophthalmically | Ketoralac |
| NSAID that is used for acute condition, such as pre-op anesthesia and has limited duration (<5 days) of use due to nephrotoxicity | Ketoralac |
| Newer NSAIDs that selectively inhibit COX-2 | Celecoxib and rofecoxib |
| COX 2 inhibitors may have reduced risk of | Gastric ulcers and GI Bleeding |
| COX 2 inhibitors should be used cautiously in pts with | Pre-existing cardiac or renal disease |
| Acetaminophen only has | Antipyretic and analgesic activity |
| SE of acetaminophen | Hepatotoxicity |
| Antidote for acetaminophen toxicity | N-acetylcysteine |
| Drugs-Modifying Anti-Rheumatic Agents (DMARDS) DMARDs are slow acting drugs for | Rheumatic disease |
| MOA of gold salts | Alter activity of macrophages and suppress phagocytic activity of PMNs |
| SE of gold salts | Dermatitis of the mouth aplastic anemia and agranulocytosis |
| Causes bone marrow suppression | Methotrexate |
| SE of penicillamine | Aplastic anemia and renal |
| Interferes with activity of T-lymphocytes | Hydroxychloroquine |
| Anti-malarial drug used in rheumatoid arthritis (RA) | Hydroxychloroquine |
| SE of hydroxychloroquine | Retinal destruction and dermatitis |
| MOA of Leflunomide (newer agent) | Inhibiting Dihydroorotate Dehydrogenase which leads to decreased pyrimidine synthesis |
| Proteins that prevent action of tumor necrosis factor alpha (TNF-alpha) | Infliximab and etanercept |
| Anti-rheumatic agent also used for ulcerative colitis | Sulfasalazine |
| Drugs used in Gout NSAIDS used in gout | Indomethacin and phenylbutazone |
| NSAID contraindicated in gout | Aspirin |
| SE of phenylbutazone | Aplastic anemia and agranulocytosis |
| MOA of Colchicine (used in acute gout) | Selective inhibitor of microtubule assembly |
| SE of colchicine | Kidney and liver toxicity |
| Agent used to treat chronic gout by increasing uric acid secretion | Probenecid and sulfinpyrazone |
| Allopurinol treats chronic gout by inhibiting | Xanthine oxidase |
Created by:
csheck
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